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MX2016004834A - PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE INHIBITOR (PDE4). - Google Patents

PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE INHIBITOR (PDE4).

Info

Publication number
MX2016004834A
MX2016004834A MX2016004834A MX2016004834A MX2016004834A MX 2016004834 A MX2016004834 A MX 2016004834A MX 2016004834 A MX2016004834 A MX 2016004834A MX 2016004834 A MX2016004834 A MX 2016004834A MX 2016004834 A MX2016004834 A MX 2016004834A
Authority
MX
Mexico
Prior art keywords
preparation
pde4
phosphodiesterase inhibitor
compound
formula
Prior art date
Application number
MX2016004834A
Other languages
Spanish (es)
Other versions
MX370104B (en
Inventor
Alessandro Falchi
Emilio Lutero
Emanuele Ferrari
Fausto Pivetti
Rocco Bussolati
Edoardo Mariani
Orsola Vecchi
Erhard Bappert
Caterina Ventrici
Original Assignee
Chiesi Farma Spa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49385193&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX2016004834(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chiesi Farma Spa filed Critical Chiesi Farma Spa
Publication of MX2016004834A publication Critical patent/MX2016004834A/en
Publication of MX370104B publication Critical patent/MX370104B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61Halogen atoms or nitro radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/49Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
    • C07C205/57Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C205/59Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Proceso para la preparación de compuestos que poseen actividad inhibitoria de fosfodiesterasa (PDE4) de fórmula (I). La invención también se relaciona con el proceso para el aislamiento por cristalización del compuesto (I) y su uso para la preparación de composiciones farmacéuticas para inhalación en combinación con transportadores o vehículos adecuados. La presente invención también se relaciona con solvatos y formas cristalinas de un compuesto de fórmula (I). El producto sintetizado es adecuado para el uso en aplicaciones farmacéuticas por ejemplo en el tratamiento de enfermedades respiratorias.Process for the preparation of compounds that possess phosphodiesterase (PDE4) inhibitory activity of formula (I). The invention also relates to the process for crystallization isolation of compound (I) and its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystalline forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for example in the treatment of respiratory diseases.

MX2016004834A 2013-10-22 2014-10-17 PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE INHIBITOR (PDE4). MX370104B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13189784 2013-10-22
PCT/EP2014/072334 WO2015059050A1 (en) 2013-10-22 2014-10-17 Process for the preparation of a pde4 inhibitor

Publications (2)

Publication Number Publication Date
MX2016004834A true MX2016004834A (en) 2016-07-19
MX370104B MX370104B (en) 2019-12-02

Family

ID=49385193

Family Applications (4)

Application Number Title Priority Date Filing Date
MX2019014408A MX389002B (en) 2013-10-22 2014-10-17 PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE (PDE4) INHIBITOR.
MX2016004834A MX370104B (en) 2013-10-22 2014-10-17 PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE INHIBITOR (PDE4).
MX2022000030A MX2022000030A (en) 2013-10-22 2016-04-14 PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE (PDE4) INHIBITOR.
MX2022000036A MX2022000036A (en) 2013-10-22 2016-04-14 Process for the preparation of a pde4 inhibitor.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2019014408A MX389002B (en) 2013-10-22 2014-10-17 PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE (PDE4) INHIBITOR.

Family Applications After (2)

Application Number Title Priority Date Filing Date
MX2022000030A MX2022000030A (en) 2013-10-22 2016-04-14 PROCESS FOR THE PREPARATION OF A PHOSPHODIESTERASE (PDE4) INHIBITOR.
MX2022000036A MX2022000036A (en) 2013-10-22 2016-04-14 Process for the preparation of a pde4 inhibitor.

Country Status (29)

Country Link
US (7) US9434691B2 (en)
EP (5) EP3293176B1 (en)
JP (5) JP6458957B2 (en)
KR (3) KR102240865B1 (en)
CN (5) CN105658629B (en)
AR (4) AR098128A1 (en)
AU (1) AU2014339136C1 (en)
BR (1) BR112016008161B1 (en)
CA (3) CA2928242C (en)
CY (1) CY1123811T1 (en)
DK (3) DK3293176T3 (en)
ES (3) ES2759514T3 (en)
FI (1) FI3587400T3 (en)
HR (3) HRP20192152T1 (en)
HU (3) HUE053112T2 (en)
IL (4) IL285528B2 (en)
LT (2) LT3293176T (en)
MX (4) MX389002B (en)
MY (1) MY182559A (en)
PH (3) PH12021550257A1 (en)
PL (3) PL3293176T3 (en)
PT (3) PT3060551T (en)
RS (2) RS65452B1 (en)
RU (1) RU2682660C9 (en)
SG (4) SG10201912852YA (en)
SI (3) SI3060551T1 (en)
TW (3) TWI651305B (en)
UA (2) UA121853C2 (en)
WO (1) WO2015059050A1 (en)

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Publication number Publication date
RU2016115246A3 (en) 2018-06-27
MY182559A (en) 2021-01-25
JP6458957B2 (en) 2019-01-30
JP7534346B2 (en) 2024-08-14
EP3587400A2 (en) 2020-01-01
AR122183A2 (en) 2022-08-24
CN120607463A (en) 2025-09-09
IL285532A (en) 2021-09-30
SI3587400T1 (en) 2024-05-31
IL285528B1 (en) 2025-05-01
IL285528A (en) 2021-09-30
US20160326117A1 (en) 2016-11-10
KR102240865B1 (en) 2021-04-16
EP4059921A1 (en) 2022-09-21
ES2759514T3 (en) 2020-05-11
TW201605804A (en) 2016-02-16
SG10201903575UA (en) 2019-05-30
HRP20210336T1 (en) 2021-04-16
MX370104B (en) 2019-12-02
TWI685486B (en) 2020-02-21
BR112016008161A2 (en) 2017-08-01
JP2017505752A (en) 2017-02-23
CA3115570C (en) 2024-01-30
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MX2022000030A (en) 2022-07-19
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AU2014339136B2 (en) 2018-05-31
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TW201904945A (en) 2019-02-01
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US20150111931A1 (en) 2015-04-23
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CN120136784A (en) 2025-06-13
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US20240166605A1 (en) 2024-05-23
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RU2016115246A (en) 2017-11-27
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CA2928242C (en) 2022-03-15
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IL252834A0 (en) 2017-08-31
US11981639B2 (en) 2024-05-14
US20180118686A1 (en) 2018-05-03
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AR118124A2 (en) 2021-09-22
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US10323003B2 (en) 2019-06-18
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IL252834B (en) 2021-09-30
SG10201912852YA (en) 2020-02-27
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LT3293176T (en) 2021-03-25
PL3587400T3 (en) 2024-07-01
JP7051970B2 (en) 2022-04-11
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